US4732914AExpiredUtility

Prostacyclin analogs

Assignee: UPJOHN COPriority: Feb 13, 1978Filed: May 14, 1987Granted: Mar 22, 1988
Est. expiryFeb 13, 1998(expired)· nominal 20-yr term from priority
C07D 257/04C07C 29/095C07C 45/60C07C 45/62C07C 45/64C07C 45/673C07C 405/0083C07D 309/12C07D 319/06C07C 2603/66C07F 7/1804
84
PatentIndex Score
20
Cited by
2
References
2
Claims

Abstract

Prostacyclin (PGI 2 ) analogs having a 6a-carba feature, for example a compound of the formula ##STR1## said analogs having pharmacological activity. Processes for preparing them and the appropriate intermediates are disclosed.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A compound of the formula I ##STR112## wherein D is (1) --(CH 2 ) d  -- wherein d is one to 5, inclusive, (2) --(CH 2 ) d  --CF 2  -- wherein d is one to 5 inclusive, (3) --(CH 2 ) k  --CH═CH-- wherein k is one or 2,     wherein Q 1  is ##STR113## wherein R 8  is hydrogen or methyl; wherein R 3  is (a) hydrogen,   (b) alkyl of one to 12 carbon atoms, inclusive,   (c) cycloalkyl of 3 to 10 carbon atoms, inclusive,   (d) aralkyl of 7 to 12 carbon atoms, inclusive,   (e) phenyl,   (f) phenyl substituted with one, 2, or 3 chloro or alkyl of one to 4 carbon atoms, inclusive ##STR114## wherein R 9  is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl, and     wherein R 10  is hydrogen or benzoyl, or (n) a pharmacologically acceptable cation;   wherein  ○R 2    is ##STR115## wherein R 43  is ##STR116## wherein C g  H 2g  is alkylene of one to 9 carbon atoms, inclusive, with one to 5 carbon atoms, inclusive, in the chain between --CR 12  R 13  -- and terminal methyl, wherein R 12  and R 13  are hydrogen, alkyl of one to 4 carbon atoms, inclusive, or fluoro, being the same or different, with the proviso that one of R 12  and R 13  is fluoro only when the other is hydrogen or fluoro; or hydrogen or fluoro; or ##STR117## wherein X is --C.tbd.C--; and wherein ˜ indicates attachment in alpha or beta configuration.   
     
     
       2. A method of inhibiting blood platelet aggregation comprising contacting said blood platelets with an effective amount of a compound of the claim 1.

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